| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
Vortioxetine lactate (formerly Lu-AA21004 lactate; Trintellix; Brintellix) is the lactate salt of Vortioxetine, which is an atypical antidepressant which was approved in 2013 by the FDA for the treatment of major depressive disorder (MDD) in adults. It has IC50 values of 15 nM, 33 nM, 3.7 nM, 19 nM, and 1.6 nM for 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor, and SERT, respectively.
| ln Vitro |
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Enzyme Assay |
Vortioxetine (Compound 5m) is a multimodal serotonergic agent that inhibits SERT with values of 1.6 nM, 33 nM, 3.7 nM, 19 nM, and 5-HT1A, 5-HT1B, and 5-HT7 receptors, respectively. Vortioxetine exhibits strong suppression of SERT as well as antagonistic effects at 5-HT3A and 5-HT7 receptors, partial agonist effects at 5-HT1B receptors, and agonistic effects at 5-HT1A receptors.
|
||
| Cell Assay |
Vortioxetine is a partial h5-HT1B receptor agonist that, in a whole-cell cAMP-based assay, has an EC50 of 460 nM and an intrinsic activity of 22%. In vitro whole-cell cAMP assay, vortioxetine binds to the r5-HT7 receptor with a Kivalue of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM.
|
||
| Animal Protocol |
|
||
| References |
| Molecular Formula |
C21H28N2O3S
|
|
|---|---|---|
| Molecular Weight |
388.526
|
|
| Exact Mass |
388.18
|
|
| CAS # |
1253056-29-9
|
|
| Related CAS # |
|
|
| SMILES |
CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C.CC(C(=O)O)O
|
|
| InChi Key |
KJXWEKCEAVJWHZ-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C18H22N2S.C3H6O3/c1-14-7-8-17(15(2)13-14)21-18-6-4-3-5-16(18)20-11-9-19-10-12-20;1-2(4)3(5)6/h3-8,13,19H,9-12H2,1-2H3;2,4H,1H3,(H,5,6)
|
|
| Chemical Name |
1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine;2-hydroxypropanoic acid
|
|
| Synonyms |
Vortioxetine lactate
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5738 mL | 12.8690 mL | 25.7380 mL | |
| 5 mM | 0.5148 mL | 2.5738 mL | 5.1476 mL | |
| 10 mM | 0.2574 mL | 1.2869 mL | 2.5738 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 |
|---|
|
 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
